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We previously identified 3-chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide (5, TP0439150) as a potent and orally available glycine transporter 1 (GlyT1) inhibitor. In this article, we describe our identification of 1-methyl-N-(propan-2-yl)-N-({2-[4-(trifluoromethoxy)phenyl]pyridin-4-yl}methyl)-1H-imidazole-4-carboxamide (7n) as a structurally diverse back-up compound of 5, using central nervous system multiparameter optimization (CNS MPO) as a drug-likeness guideline. Compound 7n showed a higher CNS MPO score and different physicochemical properties as compared to 5. Compound 7n exhibited potent GlyT1 inhibitory activity, a favorable pharmacokinetics profile, and elicited an increase in the cerebrospinal fluid (CSF) concentration of glycine in rats.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Identification of 1-Methyl-&lt;i&gt;N&lt;/i&gt;-(propan-2-yl)-&lt;i&gt;N&lt;/i&gt;-({2-[4-(trifluoromethoxy)phenyl]pyridin-4-yl}methyl)-1&lt;i&gt;H&lt;/i&gt;-imidazole-4-carboxamide as a Potent and Orally Available Glycine Transporter 1 Inhibitor